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Page 1
CSTI-300 (SMP-100); a Novel 5-HT3 Receptor Partial Agonist with Potential to Treat Patients with Irritable Bowel Syndrome or Carcinoid Syndrome.
Roberts A, Grafton G, Powell AD, Brock K, Chen C, Xie D, Huang J, Liu S, Cooper AJ, Brady CA, Qureshi O, Stamataki Z, Manning DD, Moore NA, Sargent BJ, Guzzo PR, Barnes NM. Roberts A, et al. Among authors: guzzo pr. J Pharmacol Exp Ther. 2020 Apr;373(1):122-134. doi: 10.1124/jpet.119.261008. Epub 2020 Feb 26. J Pharmacol Exp Ther. 2020. PMID: 32102919
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
Manning DD, Cioffi CL, Usyatinsky A, Fitzpatrick K, Masih L, Guo C, Zhang Z, Choo SH, Sikkander MI, Ryan KN, Naginskaya J, Hassler C, Dobritsa S, Wierschke JD, Earley WG, Butler AS, Brady CA, Barnes NM, Cohen ML, Guzzo PR. Manning DD, et al. Among authors: guzzo pr. Bioorg Med Chem Lett. 2011 Jan 1;21(1):58-61. doi: 10.1016/j.bmcl.2010.11.080. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21146988
The discovery of diazepinone-based 5-HT3 receptor partial agonists.
Manning DD, Guo C, Zhang Z, Ryan KN, Naginskaya J, Choo SH, Masih L, Earley WG, Wierschke JD, Newman AS, Brady CA, Barnes NM, Guzzo PR. Manning DD, et al. Among authors: guzzo pr. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2578-81. doi: 10.1016/j.bmcl.2014.03.074. Epub 2014 Apr 2. Bioorg Med Chem Lett. 2014. PMID: 24755431
Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1.
Cioffi CL, Liu S, Wolf MA, Guzzo PR, Sadalapure K, Parthasarathy V, Loong DT, Maeng JH, Carulli E, Fang X, Karunakaran K, Matta L, Choo SH, Panduga S, Buckle RN, Davis RN, Sakwa SA, Gupta P, Sargent BJ, Moore NA, Luche MM, Carr GJ, Khmelnitsky YL, Ismail J, Chung M, Bai M, Leong WY, Sachdev N, Swaminathan S, Mhyre AJ. Cioffi CL, et al. Among authors: guzzo pr. J Med Chem. 2016 Sep 22;59(18):8473-94. doi: 10.1021/acs.jmedchem.6b00914. Epub 2016 Sep 9. J Med Chem. 2016. PMID: 27559615 Free article.
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Liu S, Zha C, Nacro K, Hu M, Cui W, Yang YL, Bhatt U, Sambandam A, Isherwood M, Yet L, Herr MT, Ebeltoft S, Hassler C, Fleming L, Pechulis AD, Payen-Fornicola A, Holman N, Milanowski D, Cotterill I, Mozhaev V, Khmelnitsky Y, Guzzo PR, Sargent BJ, Molino BF, Olson R, King D, Lelas S, Li YW, Johnson K, Molski T, Orie A, Ng A, Haskell R, Clarke W, Bertekap R, O'Connell J, Lodge N, Sinz M, Adams S, Zaczek R, Macor JE. Liu S, et al. Among authors: guzzo pr. ACS Med Chem Lett. 2014 May 13;5(7):760-5. doi: 10.1021/ml500053b. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050161 Free PMC article.
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Liu J, He S, Jian T, Dobbelaar PH, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Pattamana K, Ruenz M, Sargent BJ, Swenson B, Yet L, Tamvakopoulos C, Peng Q, Pan J, Kan Y, Palyha O, Kelly TM, Guan XM, Howard AD, Marsh DJ, Metzger JM, Reitman ML, Wyvratt MJ, Nargund RP. Liu J, et al. Among authors: guzzo pr. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2074-7. doi: 10.1016/j.bmcl.2010.02.076. Epub 2010 Feb 21. Bioorg Med Chem Lett. 2010. PMID: 20219372
Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Hadden M, Goodman A, Guo C, Guzzo PR, Henderson AJ, Pattamana K, Ruenz M, Sargent BJ, Swenson B, Yet L, Liu J, He S, Sebhat IK, Lin LS, Tamvakopoulos C, Peng Q, Kan Y, Palyha O, Kelly TM, Guan XM, Metzger JM, Reitman ML, Nargund RP. Hadden M, et al. Among authors: guzzo pr. Bioorg Med Chem Lett. 2010 May 1;20(9):2912-5. doi: 10.1016/j.bmcl.2010.03.028. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20347296
Bifidenone: Structure-Activity Relationship and Advanced Preclinical Candidate.
Huang Z, Williams RB, Martin SM, Lawrence JA, Norman VL, O'Neil-Johnson M, Harding J, Mangette JE, Liu S, Guzzo PR, Starks CM, Eldridge GR. Huang Z, et al. Among authors: guzzo pr. J Med Chem. 2018 Aug 9;61(15):6736-6747. doi: 10.1021/acs.jmedchem.7b01644. Epub 2018 Jul 25. J Med Chem. 2018. PMID: 29995409
30 results